Opsumit
Opsumit Uses, Dosage, Side Effects, Mechanism of Action, How Long Does it Take to Work? Opsumit is a brand name. Its generic name is Macitentan.
Opsumit Introduction
Opsumit (Opsumit) is an orally administered, selective endothelin receptor antagonist (ERA) developed and marketed by Actelion on behalf of the Japanese pharmaceutical company Takeda. It is used in the treatment of pulmonary arterial hypertension (PAH). Opsumit is a dual inhibitor of endothelin-1 (ET-1) and endothelin-2 (ET-2) receptors, acting on the ETAR to decrease the production and action of ET-1, and on the ETBR to reduce the effect of ET-2. The drug has also been investigated for its potential use in other diseases in which the endothelin system is believed to be involved in pathogenesis, such as congestive heart failure, atherosclerosis, and pre-eclampsia.Opsumit Uses
Opsumit is indicated for the treatment of pulmonary arterial hypertension (PAH). This includes individuals with WHO Functional Class II-IV symptoms of PAH. Additionally, Opsumit (Opsumit) has been investigated for its potential use in other diseases in which the endothelin system is believed to be involved in pathogenesis, such as congestive heart failure, atherosclerosis, and pre-eclampsia.Opsumit Mechanism of Action
Opsumit functions as a dual inhibitor of the endothelin-1 (ET-1) and endothelin-2 (ET-2) receptors, acting on the ETAR to decrease the production and action of ET-1, and on the ETBR to reduce the effect of ET-2. The drug also reduces the expression of pro-fibrotic genes, leading to an attenuation of fibrosis in pulmonary arterial endothelium. Opsumite also increases the interactions between pulmonary arterial endothelial cells and smooth muscle cells, leading to an important contribution to the maintenance of the wall of the pulmonary arterial vessels.How Long does it Take for Opsumit to Work?
The onset of action varies depending on individual patient characteristics. Generally, Opsumit is expected to start working within 1-4 weeks; however, some patients may notice an effect as early as 1 week.Opsumit Absorption
Opsumit is rapidly absorbed from the gastrointestinal tract, with peak plasma concentrations achieved after 1-2 hours, with a bioavailability of approximately 100%. The drug is highly bound to plasma proteins (approximately 98%).Opsumit Route of Elimination
The primary route of elimination of Opsumit is through metabolism via CYP2C9 and, to a lesser extent, CYP2C8 and CYP2C19. After metabolism, the drug is mainly eliminated via renal excretion in bile acids and feces.Opsumit Dosage
The recommended dose of Opsumit is 10 mg once daily. It can be taken with or without food. Unless there is an intolerance or contraindication, Opsumit should be taken at the same time each day.Opsumit Administration
Opsumit is administered orally, through tablets. It should be taken with a full glass of water. Patients should not chew, divide, or crush the tablets.Opsumit Side Effects
The most commonly reported side effects of Opsumit include headache, diarrhea, nasopharyngitis, back pain, and an increase in liver enzymes. Other rarer but more serious side effects may include anemia, serious skin reactions, and liver damage.Opsumit Toxicity
There is a potential for serious toxicity if Opsumit is taken in overdose. Symptoms of toxicity include headache, dizziness, nausea, vomiting, diarrhea, abdominal pain, and hypotension. Treatment of overdose includes symptomatic and supportive care as needed.Opsumit Precaution
Patients should be monitored closely for liver function, blood pressure, and symptoms of toxicity. Opsumit should not be used in combination with other endothelin receptor antagonists or in patients with known hypersensitivity to the drug.Opsumit Interaction
Opsumit may interact with strong CYP2C8 and CYP2C9 inducers or inhibitors, as well as drugs that are known to prolong the QT interval. Opsumit should be used with caution in patients taking other drugs that may have similar effects.Opsumit Disease Interactions
Opsumit is contraindicated in patients with severe hepatic impairment. Use with caution in patients with mild-to-moderate hepatic impairment and in those with a history of hepatic impairment. Use should be avoided in patients with moderate-to-severe renal impairment.Opsumit Drug Interactions
Opsumit may interact with strong CYP2C8 and CYP2C9 inducers or inhibitors, as well as drugs that are known to prolong the QT interval. Opsumit should be used with caution in patients taking other drugs that may have similar effects.Opsumit Food Interactions
Opsumit should not be taken with food that is high in fat as this may decrease the absorption of Opsumit. Grapefruit juice should be avoided as this may increase the amount of Opsumit that is absorbed in the body.Opsumit Pregnancy Use
Opsumit is not recommended for use in pregnant women. There is no data on the use of Opsumit in pregnant animals. Animal studies have shown reproductive toxicity.Opsumit Lactation Use
Neither Opsumit nor any of its metabolites have been detected in human milk. However, a clinical decision should be made about whether to discontinue breastfeeding based on the importance of the drug to the mother.Opsumit Acute Overdose
In the event of an acute overdose of Opsumit, the patient should be monitored for signs and symptoms of toxicity and supportive care should be given as needed.Opsumit Contraindication
Opsumit is contraindicated in patients with severe hepatic impairment and in those with known hypersensitivity to the drug. It should also be used with caution in patients with mild-to-moderate hepatic impairment and in those taking other drugs that may have similar effects.Opsumit Use Direction
The recommended dose of Opsumit is 10 mg once daily. It can be taken with or without food. Unless there is an intolerance or contraindication, Opsumit should be taken at the same time each day.Opsumit Storage Condition
Opsumit should be stored at room temperature away from light and moisture. Do not store it in the bathroom. Keep the container tightly closed when not in use.Opsumit Volume of Distribution
The volume of distribution of Opsumit is 4.6 L/kg.Opsumit Half-Life
The half-life of Opsumit is approximately 7.2 hours.Opsumit Clearance
The clearance of Opsumit is 1.3 L/h/kg.Here you find in details version of Opsumit
Some Frequently Asked Questions About Opsumit
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